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    • 5. 发明授权
    • Process for the production of 1,2,4-triazin-5-one derivatives
    • 制备1,2,4-三嗪-5-酮衍生物的方法
    • US4175188A
    • 1979-11-20
    • US924062
    • 1978-07-12
    • Herbert KlenkWerner SchwarzeWolfgang Leuchtenberger
    • Herbert KlenkWerner SchwarzeWolfgang Leuchtenberger
    • C07D253/06A01N43/707C07D253/075
    • C07D253/075A01N43/707
    • 1,2,4-triazin-5-one compounds of the general formula (I) ##STR1## where R is ##STR2## are prepared by reacting a compound of general formula (II) ##STR3## in which R is defined above with either (a) a tertiary alcohol of general formula (III)HO--R' (III) in which R' is a t-alkyl group having 4 to 18 carbon atoms, especially t-amyl or t-octyl or preferably t-butyl or(b) an alkene of general formula (IV) ##STR4## in which R.sub.1 and R.sub.2 are the same or different and are hydrogen or an alkyl group and R.sub.3 and R.sub.4 are the same or different and wherein the alkyl groups in each case can be 1 to 15 carbon atoms and wherein preferably R.sub.1 and R.sub.2 are hydrogen and R.sub.3 and R.sub.4 each are methyl to form an .alpha.-ketocarboxylic acid amide of general formula (V) ##STR5## and this, in a given case after previous saponification to the free acid, condensed with thiocarbohydrazide ##STR6## to form a 1,2,4-triazin-5-one compound of general formula (VI) ##STR7## and then the mercapto group is methylated.
    • 通式(I)的化合物通过使通式(II)的化合物(II)的化合物在 其中R定义如上:(a)通式(III)的叔醇HO-R'(III),其中R'是具有4至18个碳原子的叔烷基,特别是叔戊基或t- 辛基或优选叔丁基或(b)通式(IV)的烯烃其中R 1和R 2相同或不同,为氢或烷基,且R 3和R 4相同或不同 并且其中每种情况下的烷基可以是1至15个碳原子,并且其中优选地,R 1和R 2是氢,并且R 3和R 4各自是甲基,形成通式(V)的α-酮羧酸酰胺。 并且在给定情况下,在先前皂化成游离酸后,与硫代碳酰肼“IMAGE”缩合形成通式(VI)的化合物VI(VI),然后 巯基是甲基 ted。